I. Field of the Invention
The present invention generally relates to therapeutic compositions and formulations with catechol. More particularly, the present invention relates to an oral medicament, a dietary supplement, a nutritional supplement, a food supplement, a food additive, a pharmaceutical, a nutraceutical, or nutratherapeutical formulations that include antioxidant, anticancer, antiviral and anti-rheumatic properties. The compositions and formulations demonstrate positive effects against a broad variety of cancers, autoimmune and rheumatological diseases, and provide antioxidant protection against peroxyl radicals of both the hydrophillic and the lipophilic types, hydroxyl radicals, peroxynitrite radicals and super oxide radicals.
II. Description of the Relevant Art
Cancer is one of the leading causes of death and incidences of this devastating disease are on the rise all over the world virtually afflicting every family. Attempts have been made to provide a nutra-therapeutical chemotherapeutic agent with selective activity against a broad variety of cancer cells, without the known side effects associated with orthodox chemotherapeutic agents. The proponents of these attempts believed that the known formulas for such a nutratherapeutical possessed such therapeutic properties. Furthermore, it was believed that a multitude of active ingredients existing in a necessary and precise ratio was the source of the purported anticancer activity. However, NCI, FDA and ACS, have determined that the known compositions had no effect against cancer.
Autoimmune disease or rheumatoid disorder is a pathological condition, in which a patient's normal antibodies no longer recognize its own tissues as self; and thereby attacks and breaks down these tissues. A high rheumatoid factor may lead to autoimmune and rheumatoid diseases, which diseases include lupus, erythematosus, rheumatoid arthritis, rheumatism, scleroderma, gout, polymyalgia rheumatica, fibromyalgia, ankylosing spondylitis, and osteoarthritis.
It is well known that free radicals are chemically reactive molecules that damage cellular structure and function. Free radicals are oxidants that damage and destroy healthy cells. Oxygen-based free radicals include peroxyls (ROO−) of the water soluble (hydrophilic) and fat soluble (lipophilic) types, superoxide anions (O2−), peroxynitrites (ONNO−) and hydroxyls (—OH). Sources of free radicals include ultraviolet radiation, carcinogens, and high-fat processed foods. It is also known that physical stress and even normal cell function in the production of energy are both sources for the creation and release of free radicals. A broad variety of disease states have been linked to the presence of free radicals, including arthritis, cancer, heart dysfunction, atherosclerosis, hyperoxia, stroke, cataractogenesis, retinal damage, liver injury, sexual dysfunction, periodontis, vasospasms, dermatitis, and asthma.
In response to the overwhelming presence of oxygen-based free radicals in our natural environment, attention has focused on antioxidants, compounds that can inhibit the cellular damage caused by free radicals. Natural sources of antioxidants are known and include vitamins C and E, broccoli, alpha-Lipoic acid, grapeseed, and green tea extract. While offering an avenue to obtaining the positive effects of antioxidants, the dosages of these natural foods needed to offset the oxidants is extremely high.
Attempts have also been made to provide concentrated antioxidants as a dietary supplement, a food supplement, a nutritional supplement, a food additive, a pharmaceutical, a nutraceutical, or a nutra-therapeutical according to various formulations; which contain antioxidant, anticancer, anti-viral and anti-rheumatoid properties. Each of these formulations included tetrahydroxy-1,4-quinone (C6H4O6) (hereinafter referred to occasionally as “THQ”) (in its free form and its sulfited form), croconic acid (in its free form and its sulfited form), and catechol (pyrocatechol) as active ingredients. These formulations have gone by various names, including “Entelev®,” “Cantron®” (in three versions), “Cancell®,” and “Protocel®” (in three versions). Perhaps the best known of these early attempts at providing an effective anti-cancer, antioxidant, anti-rheumatic and anti-viral formulation is the “Cantron®” composition which had, in addition to catechol, varied amounts of croconic acid (in its free form and its sulfited form), THQ (in its free form and its sulfited form) and rhodozonic acid, the latter converting in part to croconic acid (in its free form and its sulfited form) during the formulation process. Various additional ingredients to these formulations include sulfur, sodium, copper, potassium, triquinoyl, leuconic acid, hexahydrabenzene and traces of inositol.
While providing some improvement in the state of the art, these formulations have not proven either fully effective or completely desirable. These shortcomings include unmanageable and inadequate dosing requirements, undesirable physical characteristics of the composition, and safety issues related to the manufacturing process.
Dosage management has been a problem with these compositions in that the liquid of known formulations needed to be four to five times per day. Furthermore, new findings described herein indicate optimum dosage requirements are now every 1-2 hours; an extremely difficult schedule to follow even under the best of circumstances.
The physical characteristics of known formulations also make use of these compositions problematic. Specifically, the known compositions are designed to be orally ingested. However, the oral liquid has an extremely foul metallic taste and often burns or irritates mouth tissues. Users historically found the composition unappetizing, this problem being compounded by the user's need to consume the composition four or five times daily or optimally every one to two hours. Some users find the taste so unappealing that it causes nausea in many instances. Nausea is an undesirable characteristic even in the best of circumstances but even more undesirable for cancer patients who already may be exhibiting nausea due to the nature of the illness of from ingesting standard chemotherapeutic agents. Nine out of ten users abandon use of the known composition as a result of the adverse taste despite facing severe health challenges and in dire need of treatment. Virtually no person is willing to take this formulation on a prophylactic basis because of taste issues. This not only renders a situation with poor patient compliance but it also makes for a poor product in the marketplace.
Beyond taste, the dark black liquid of known compositions is itself visually unappealing. The color of the known compositions is known to stain teeth, clothing, furniture, and carpeting. The stains on clothing, furniture and carpeting are permanent as well as in the case of porous teeth. The problem is further compounded by the difficulty of traveling with these bulky liquid compositions. The container top is subject to loosening because of the gases naturally generated by the composition and causes leakage which is problematic for shipping or traveling because the dark black liquid destroys all other products contained in a shipping container or in baggage whereby it permanently damages clothing and other valuable items.
Of concern to manufacturers is the production process itself. The manufacturing procedure of the formula is extremely dangerous as the oxidation process to create the various compounds causes the release of a highly toxic and acidic gas. Experience has taught that the larger the volume of product being produced, the more dangerous the chemical reaction. So dangerous is the manufacturing procedure for known compositions that production on a large scale may lead to injury or death, which is the reason that previous manufacturing has been done on a small scale only. Because of the level of pernicious nitric fumes generated, even protective wear that would ordinarily be effective (such as gas masks) fail to protect the operator. Furthermore, experience has shown that stove wiring, fan motors, vacuum motors and general laboratory equipment must be renewed constantly and at considerable expense due to the presence of these acidic gases. In addition, laboratory cleanliness is all but impossible to maintain given the presence of these gases, resulting in stained walls, floors and furniture. So extreme is the problem that to maintain laboratory cleanliness at even the most rudimentary level the walls must be recoated with paint after the production of each batch. Given these problems, FDA or regulatory authority inspection compliance has been problematic.
Beyond the difficulties associated with the production of known compositions, the known compositions have a variety of demonstrable shortcomings. First, prior compositions fail to produce an optimum effect in that they do not utilize the most effective administration methods or dosages. Second, known compositions are unsafe to manufacture in any significant quantity. Third, known compositions have a black, tarry appearance and are unappealing to the user in appearance. Fourth, known compositions are unappealing to the user in taste.
Accordingly, new compositions and improved formulations that demonstrate higher antioxidant characteristics on the major oxygen related species of free radicals, increased efficacy against a broad variety of cancers, autoimmune diseases such as lupus and rheumatoid arthritis and a broad array of viruses (including for example, the AIDS virus) while allowing safe manufacture and appeal to the user are desired.